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叶酸修饰的 TPGS 作为一种新型纳米胶束，用于递送盐酸小檗碱，以提高 Huh7 人肝癌细胞的凋亡诱导作用。

Folic acid modified TPGS as a novel nano-micelle for delivery of nitidine chloride to improve apoptosis induction in Huh7 human hepatocellular carcinoma.

机构信息

School of Chemistry and chemical engineering, Guangxi Key Laboratory for Polysaccharide Materials and Modifications, Guangxi University for nationalities, No.158, Da Xue Xi street, Xixiangtang District, Nanning, 530006, Guangxi Province, China.

College of Pharmacy, Guangxi University for Chinese medicine, No.13, Wu He street, Qingxiu District, Nanning, 530200, Guangxi Province, China.

出版信息

BMC Pharmacol Toxicol. 2021 Jan 6;22(1):1. doi: 10.1186/s40360-020-00461-y.

DOI:10.1186/s40360-020-00461-y
PMID:33407916
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7789002/
Abstract

BACKGROUND

The development of novel and effective drugs for targeted human hepatocellular carcinoma still remains a great challenge. The alkaloid nitidine chloride (NC), a component of a traditional Chinese medicine, has been shown to have anticancer properties, but doses at therapeutic levels have unacceptable side effects. Here we investigate folic acid modified D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS-FA) as a potential carrier for controlled delivery of the drug.

METHODS

Synthesized TPGS-FA was characterized by FTIR, UV-visible and H NMR spectroscopy, and TPGS loaded with NC was evaluated for its ability to induce apoptosis in Huh7 cells by Annexin V/PI and MTT assays, and observed by laser scanning confocal microscopy and inverted phase contrast microscopy.

RESULTS

TPGS-FA/NC complexes were prepared successfully, and were homogenious with a uniform size of ~ 14 nm diameter. NC was released from the TPGS-FA/NC complexes in a controlled and sustained manner under physiological conditions (pH 7.4). Furthermore, its cytotoxicity to hepatocarcinoma cells was greater than that of free NC.

CONCLUSIONS

TPGS-FA is shown to be useful carrier for drugs such as NC, and TPGS-FA/NC could potentially be a potent and safe drug for the treatment of hepatocellular carcinoma.

摘要

背景

开发针对人类肝细胞癌的新型有效药物仍然是一个巨大的挑战。生物碱硝酸氯（NC）是一种中药的成分，已被证明具有抗癌特性，但治疗水平的剂量有不可接受的副作用。在这里，我们研究叶酸修饰的 D-α-生育酚聚乙二醇 1000 琥珀酸酯（TPGS-FA）作为药物控制递送的潜在载体。

方法

通过傅里叶变换红外光谱（FTIR）、紫外-可见光谱和 H 核磁共振光谱对合成的 TPGS-FA 进行了表征，并通过 Annexin V/PI 和 MTT 测定法评估了 TPGS 负载 NC 诱导 Huh7 细胞凋亡的能力，通过激光扫描共聚焦显微镜和倒置相差显微镜进行观察。

结果

成功制备了 TPGS-FA/NC 复合物，其粒径均匀，约为 14nm。在生理条件（pH 7.4）下，NC 从 TPGS-FA/NC 复合物中以受控和持续的方式释放。此外，其对肝癌细胞的细胞毒性大于游离 NC。

结论

TPGS-FA 被证明是 NC 等药物的有用载体，TPGS-FA/NC 可能是治疗肝细胞癌的一种有效且安全的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/afc6b4b72978/40360_2020_461_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/bbf7a32e6ea3/40360_2020_461_Sch1_HTML.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/1841c8af758b/40360_2020_461_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/f7e33d53a5e8/40360_2020_461_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/09ee2aa0d6da/40360_2020_461_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/cbb4c5f01973/40360_2020_461_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/165a51342ac2/40360_2020_461_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/4723d444a333/40360_2020_461_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/a417dc320634/40360_2020_461_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/afc6b4b72978/40360_2020_461_Fig10_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/bbf7a32e6ea3/40360_2020_461_Sch1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/b817ba139f70/40360_2020_461_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/72e186edab28/40360_2020_461_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/1841c8af758b/40360_2020_461_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/f7e33d53a5e8/40360_2020_461_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/09ee2aa0d6da/40360_2020_461_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/cbb4c5f01973/40360_2020_461_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/165a51342ac2/40360_2020_461_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/4723d444a333/40360_2020_461_Fig8_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/a417dc320634/40360_2020_461_Fig9_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd84/7789002/afc6b4b72978/40360_2020_461_Fig10_HTML.jpg

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